{"title":"<i>In situ</i> gastric floating gel of atazanavir sulphate for sustained release: formulation, optimization and evaluation.","authors":"Rajashree Masareddy, Pradnya Sandure, Archana Patil, Yadishma Gaude, Arpana Patil","doi":"10.4155/tde-2023-0037","DOIUrl":null,"url":null,"abstract":"<p><p><b>Aim:</b> Atazanavir sulphate belongs to BCS class II drug, its oral bioavailability is limited due to its rapid first-pass metabolism and P-gp efflux. <b>Materials & methods:</b> The <i>in situ</i> floating gel using the complexed drug was prepared by ion gelation method and optimized the formulation as per 3<sup>2</sup> full factorial design. <b>Results:</b> Floating lag time of optimized formulation was found to be 18 s and percentage drug release of 94.18 ± 0.18 % at the end of 16 h. The concentration of gelling polymer affects drug release and a floating lag time and <i>vice versa</i>. <b>Conclusion:</b> <i>In situ</i> floating gel of atazanavir sulphate was found promising to sustain drug release due to an increased gastric residence time, which leads to enhanced potential therapy.</p>","PeriodicalId":22959,"journal":{"name":"Therapeutic delivery","volume":" ","pages":"619-633"},"PeriodicalIF":3.0000,"publicationDate":"2023-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Therapeutic delivery","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.4155/tde-2023-0037","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2023/12/6 0:00:00","PubModel":"Epub","JCR":"Q2","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
引用次数: 0
Abstract
Aim: Atazanavir sulphate belongs to BCS class II drug, its oral bioavailability is limited due to its rapid first-pass metabolism and P-gp efflux. Materials & methods: The in situ floating gel using the complexed drug was prepared by ion gelation method and optimized the formulation as per 32 full factorial design. Results: Floating lag time of optimized formulation was found to be 18 s and percentage drug release of 94.18 ± 0.18 % at the end of 16 h. The concentration of gelling polymer affects drug release and a floating lag time and vice versa. Conclusion:In situ floating gel of atazanavir sulphate was found promising to sustain drug release due to an increased gastric residence time, which leads to enhanced potential therapy.
期刊介绍:
Delivering therapeutics in a way that is right for the patient - safe, painless, reliable, targeted, efficient and cost effective - is the fundamental aim of scientists working in this area. Correspondingly, this evolving field has already yielded a diversity of delivery methods, including injectors, controlled release formulations, drug eluting implants and transdermal patches. Rapid technological advances and the desire to improve the efficacy and safety profile of existing medications by specific targeting to the site of action, combined with the drive to improve patient compliance, continue to fuel rapid research progress. Furthermore, the emergence of cell-based therapeutics and biopharmaceuticals such as proteins, peptides and nucleotides presents scientists with new and exciting challenges for the application of therapeutic delivery science and technology. Successful delivery strategies increasingly rely upon collaboration across a diversity of fields, including biology, chemistry, pharmacology, nanotechnology, physiology, materials science and engineering. Therapeutic Delivery recognizes the importance of this diverse research platform and encourages the publication of articles that reflect the highly interdisciplinary nature of the field. In a highly competitive industry, Therapeutic Delivery provides the busy researcher with a forum for the rapid publication of original research and critical reviews of all the latest relevant and significant developments, and focuses on how the technological, pharmacological, clinical and physiological aspects come together to successfully deliver modern therapeutics to patients. The journal delivers this essential information in concise, at-a-glance article formats that are readily accessible to the full spectrum of therapeutic delivery researchers.